Rapid bioluminescence assay for monitoring rat CES1 activity and its alteration by traditional Chinese medicines
In traditional Chinese medicine herbs (TCM), including Radix Salviae Miltiorrhizae (Danshen), Radix Puerariae Lobatae (Gegen), Radix Angelicae Sinensis (Danggui), and Rhizoma Chuanxiong (Chuanxiong) are widely used for the prevention and treatment of cardiovascular diseases and also often co-adminis...
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doaj-95db5b0154204c27884aac65e576a35d2021-04-02T11:33:13ZengElsevierJournal of Pharmaceutical Analysis2095-17792020-06-01103253262Rapid bioluminescence assay for monitoring rat CES1 activity and its alteration by traditional Chinese medicinesJun Zhang0Dandan Wang1Liwei Zou2Min Xiao3Yufeng Zhang4Ziwei Li5Ling Yang6Guangbo Ge7Zhong Zuo8School of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong, ChinaInstitute of Interdisciplinary Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, ChinaInstitute of Interdisciplinary Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, ChinaSchool of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong, ChinaSchool of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong, ChinaSchool of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong, ChinaInstitute of Interdisciplinary Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, ChinaInstitute of Interdisciplinary Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, ChinaSchool of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong, China; Corresponding author.In traditional Chinese medicine herbs (TCM), including Radix Salviae Miltiorrhizae (Danshen), Radix Puerariae Lobatae (Gegen), Radix Angelicae Sinensis (Danggui), and Rhizoma Chuanxiong (Chuanxiong) are widely used for the prevention and treatment of cardiovascular diseases and also often co-administered with Western drugs as a part of integrative medicine practice. Carboxylesterase 1 (CES1) plays a pivotal role in the metabolisms of pro-drugs. Since (S)-2-(2-(6-dimethylamino)-benzothiazole)-4,5-dihydro-thiazole-4-carboxylate (NLMe) has recently been identified by us as a selective CES1 bioluminescent sensor, we developed a rapid method using this substrate for the direct measurement of CES1 activity in rats. This bioluminescence assay was applied to determine CES1 activity in rat tissues after a two-week oral administration of each of the four herbs noted above. The results demonstrated the presence of CES1 enzyme in rat blood and all tested tissues with much higher enzyme activity in the blood, liver, kidney and heart than that in the small intestine, spleen, lung, pancreas, brain and stomach. In addition, the four herbs showed tissue-specific effects on rat CES1 expression. Based on the CES1 biodistribution and its changes after treatment in rats, the possibility that Danshen, Gegen and Danggui might alter CES1 activities in human blood and kidney should be considered. In summary, a selective and sensitive bioluminescence assay was developed to rapidly evaluate CES1 activity and the effects of orally administered TCMs in rats.http://www.sciencedirect.com/science/article/pii/S2095177919310743Traditional Chinese medicinesCarboxylesterase 1 (CES1)NLMeBioluminescence assayBiomatrice in rats |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Jun Zhang Dandan Wang Liwei Zou Min Xiao Yufeng Zhang Ziwei Li Ling Yang Guangbo Ge Zhong Zuo |
spellingShingle |
Jun Zhang Dandan Wang Liwei Zou Min Xiao Yufeng Zhang Ziwei Li Ling Yang Guangbo Ge Zhong Zuo Rapid bioluminescence assay for monitoring rat CES1 activity and its alteration by traditional Chinese medicines Journal of Pharmaceutical Analysis Traditional Chinese medicines Carboxylesterase 1 (CES1) NLMe Bioluminescence assay Biomatrice in rats |
author_facet |
Jun Zhang Dandan Wang Liwei Zou Min Xiao Yufeng Zhang Ziwei Li Ling Yang Guangbo Ge Zhong Zuo |
author_sort |
Jun Zhang |
title |
Rapid bioluminescence assay for monitoring rat CES1 activity and its alteration by traditional Chinese medicines |
title_short |
Rapid bioluminescence assay for monitoring rat CES1 activity and its alteration by traditional Chinese medicines |
title_full |
Rapid bioluminescence assay for monitoring rat CES1 activity and its alteration by traditional Chinese medicines |
title_fullStr |
Rapid bioluminescence assay for monitoring rat CES1 activity and its alteration by traditional Chinese medicines |
title_full_unstemmed |
Rapid bioluminescence assay for monitoring rat CES1 activity and its alteration by traditional Chinese medicines |
title_sort |
rapid bioluminescence assay for monitoring rat ces1 activity and its alteration by traditional chinese medicines |
publisher |
Elsevier |
series |
Journal of Pharmaceutical Analysis |
issn |
2095-1779 |
publishDate |
2020-06-01 |
description |
In traditional Chinese medicine herbs (TCM), including Radix Salviae Miltiorrhizae (Danshen), Radix Puerariae Lobatae (Gegen), Radix Angelicae Sinensis (Danggui), and Rhizoma Chuanxiong (Chuanxiong) are widely used for the prevention and treatment of cardiovascular diseases and also often co-administered with Western drugs as a part of integrative medicine practice. Carboxylesterase 1 (CES1) plays a pivotal role in the metabolisms of pro-drugs. Since (S)-2-(2-(6-dimethylamino)-benzothiazole)-4,5-dihydro-thiazole-4-carboxylate (NLMe) has recently been identified by us as a selective CES1 bioluminescent sensor, we developed a rapid method using this substrate for the direct measurement of CES1 activity in rats. This bioluminescence assay was applied to determine CES1 activity in rat tissues after a two-week oral administration of each of the four herbs noted above. The results demonstrated the presence of CES1 enzyme in rat blood and all tested tissues with much higher enzyme activity in the blood, liver, kidney and heart than that in the small intestine, spleen, lung, pancreas, brain and stomach. In addition, the four herbs showed tissue-specific effects on rat CES1 expression. Based on the CES1 biodistribution and its changes after treatment in rats, the possibility that Danshen, Gegen and Danggui might alter CES1 activities in human blood and kidney should be considered. In summary, a selective and sensitive bioluminescence assay was developed to rapidly evaluate CES1 activity and the effects of orally administered TCMs in rats. |
topic |
Traditional Chinese medicines Carboxylesterase 1 (CES1) NLMe Bioluminescence assay Biomatrice in rats |
url |
http://www.sciencedirect.com/science/article/pii/S2095177919310743 |
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